PL200525B1 - Zastosowanie baklofenu do wytwarzania leku - Google Patents

Zastosowanie baklofenu do wytwarzania leku

Info

Publication number: PL200525B1
Authority: PL; Poland
Prior art keywords: alcohol; baclofen; rats; treatment; administration
Prior art date: 1999-10-08

Application number

PL354083A

Other languages

English (en)

Polish (pl)

Other versions

PL354083A1 (en

Inventor

Gian Luigi Gessa

Giancarlo Colombo

Giovanni Addolorato

Original Assignee

Neuroscienze S C A R L

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

1999-10-08

Filing date

2000-10-05

Publication date

2009-01-30

2000-10-05 Application filed by Neuroscienze S C A R L filed Critical Neuroscienze S C A R L

2003-12-29 Publication of PL354083A1 publication Critical patent/PL354083A1/xx

2009-01-30 Publication of PL200525B1 publication Critical patent/PL200525B1/pl

Links

KPYSYYIEGFHWSV-UHFFFAOYSA-N Baclofen Chemical compound OC(=O)CC(CN)C1=CC=C(Cl)C=C1 KPYSYYIEGFHWSV-UHFFFAOYSA-N 0.000 title claims abstract description 54
229960000794 baclofen Drugs 0.000 title claims abstract description 54
238000011282 treatment Methods 0.000 title claims abstract description 20
208000007848 Alcoholism Diseases 0.000 title claims abstract description 13
201000007930 alcohol dependence Diseases 0.000 title claims abstract description 11
239000003814 drug Substances 0.000 claims abstract description 13
238000004519 manufacturing process Methods 0.000 claims abstract description 5
241000282414 Homo sapiens Species 0.000 claims description 5
229940079593 drug Drugs 0.000 abstract description 10
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 54
235000019441 ethanol Nutrition 0.000 description 54
241000700159 Rattus Species 0.000 description 43
230000000694 effects Effects 0.000 description 24
208000029650 alcohol withdrawal Diseases 0.000 description 14
206010010904 Convulsion Diseases 0.000 description 10
208000024891 symptom Diseases 0.000 description 10
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 10
241001465754 Metazoa Species 0.000 description 7
230000009467 reduction Effects 0.000 description 7
238000002474 experimental method Methods 0.000 description 5
231100000566 intoxication Toxicity 0.000 description 5
230000035987 intoxication Effects 0.000 description 5
206010053164 Alcohol withdrawal syndrome Diseases 0.000 description 4
206010044565 Tremor Diseases 0.000 description 4
238000000540 analysis of variance Methods 0.000 description 4
238000001647 drug administration Methods 0.000 description 4
239000000243 solution Substances 0.000 description 4
230000004580 weight loss Effects 0.000 description 4
241000700157 Rattus norvegicus Species 0.000 description 3
206010039897 Sedation Diseases 0.000 description 3
FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 3
208000007271 Substance Withdrawal Syndrome Diseases 0.000 description 3
230000001419 dependent effect Effects 0.000 description 3
231100000673 dose–response relationship Toxicity 0.000 description 3
230000036541 health Effects 0.000 description 3
238000000034 method Methods 0.000 description 3
230000036280 sedation Effects 0.000 description 3
239000011780 sodium chloride Substances 0.000 description 3
239000008399 tap water Substances 0.000 description 3
235000020679 tap water Nutrition 0.000 description 3
238000012360 testing method Methods 0.000 description 3
206010012335 Dependence Diseases 0.000 description 2
238000000729 Fisher's exact test Methods 0.000 description 2
241000282412 Homo Species 0.000 description 2
206010021703 Indifference Diseases 0.000 description 2
206010029897 Obsessive thoughts Diseases 0.000 description 2
238000003639 Student–Newman–Keuls (SNK) method Methods 0.000 description 2
206010048010 Withdrawal syndrome Diseases 0.000 description 2
238000010171 animal model Methods 0.000 description 2
210000004369 blood Anatomy 0.000 description 2
239000008280 blood Substances 0.000 description 2
230000008859 change Effects 0.000 description 2
235000019788 craving Nutrition 0.000 description 2
230000003247 decreasing effect Effects 0.000 description 2
239000012530 fluid Substances 0.000 description 2
230000037406 food intake Effects 0.000 description 2
102000006640 gamma-Glutamyltransferase Human genes 0.000 description 2
238000011670 long-evans rat Methods 0.000 description 2
238000005259 measurement Methods 0.000 description 2
239000008194 pharmaceutical composition Substances 0.000 description 2
230000002747 voluntary effect Effects 0.000 description 2
239000002023 wood Substances 0.000 description 2
RTHCYVBBDHJXIQ-MRXNPFEDSA-N (R)-fluoxetine Chemical compound O([C@H](CCNC)C=1C=CC=CC=1)C1=CC=C(C(F)(F)F)C=C1 RTHCYVBBDHJXIQ-MRXNPFEDSA-N 0.000 description 1
YSUNOHPTERXNIV-UHFFFAOYSA-N 4-amino-2-(4-chlorophenyl)butanoic acid Chemical compound NCCC(C(O)=O)C1=CC=C(Cl)C=C1 YSUNOHPTERXNIV-UHFFFAOYSA-N 0.000 description 1
102100036475 Alanine aminotransferase 1 Human genes 0.000 description 1
108010082126 Alanine transaminase Proteins 0.000 description 1
108010003415 Aspartate Aminotransferases Proteins 0.000 description 1
102000004625 Aspartate Aminotransferases Human genes 0.000 description 1
206010003591 Ataxia Diseases 0.000 description 1
206010052804 Drug tolerance Diseases 0.000 description 1
206010013754 Drug withdrawal syndrome Diseases 0.000 description 1
241001539473 Euphoria Species 0.000 description 1
206010015535 Euphoric mood Diseases 0.000 description 1
108020004206 Gamma-glutamyltransferase Proteins 0.000 description 1
101710107035 Gamma-glutamyltranspeptidase Proteins 0.000 description 1
101710173228 Glutathione hydrolase proenzyme Proteins 0.000 description 1
206010064950 Head titubation Diseases 0.000 description 1
206010019233 Headaches Diseases 0.000 description 1
206010021118 Hypotonia Diseases 0.000 description 1
241000282560 Macaca mulatta Species 0.000 description 1
241000699670 Mus sp. Species 0.000 description 1
208000008238 Muscle Spasticity Diseases 0.000 description 1
206010049816 Muscle tightness Diseases 0.000 description 1
208000002033 Myoclonus Diseases 0.000 description 1
206010062519 Poor quality sleep Diseases 0.000 description 1
AFCGFAGUEYAMAO-UHFFFAOYSA-N acamprosate Chemical compound CC(=O)NCCCS(O)(=O)=O AFCGFAGUEYAMAO-UHFFFAOYSA-N 0.000 description 1
229960004047 acamprosate Drugs 0.000 description 1
239000002253 acid Substances 0.000 description 1
230000001476 alcoholic effect Effects 0.000 description 1
230000007529 anxiety like behavior Effects 0.000 description 1
230000036528 appetite Effects 0.000 description 1
235000019789 appetite Nutrition 0.000 description 1
230000006399 behavior Effects 0.000 description 1
239000000090 biomarker Substances 0.000 description 1
230000037396 body weight Effects 0.000 description 1
210000003169 central nervous system Anatomy 0.000 description 1
230000001684 chronic effect Effects 0.000 description 1
150000001875 compounds Chemical class 0.000 description 1
230000036461 convulsion Effects 0.000 description 1
238000007405 data analysis Methods 0.000 description 1
229960003529 diazepam Drugs 0.000 description 1
AAOVKJBEBIDNHE-UHFFFAOYSA-N diazepam Chemical compound N=1CC(=O)N(C)C2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 AAOVKJBEBIDNHE-UHFFFAOYSA-N 0.000 description 1
230000008034 disappearance Effects 0.000 description 1
230000004590 drinking behavior Effects 0.000 description 1
206010013663 drug dependence Diseases 0.000 description 1
230000002255 enzymatic effect Effects 0.000 description 1
238000006911 enzymatic reaction Methods 0.000 description 1
210000003743 erythrocyte Anatomy 0.000 description 1
238000011156 evaluation Methods 0.000 description 1
229960002464 fluoxetine Drugs 0.000 description 1
235000013305 food Nutrition 0.000 description 1
235000012631 food intake Nutrition 0.000 description 1
BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical class NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 description 1
230000002496 gastric effect Effects 0.000 description 1
231100001261 hazardous Toxicity 0.000 description 1
231100000869 headache Toxicity 0.000 description 1
230000002401 inhibitory effect Effects 0.000 description 1
230000000977 initiatory effect Effects 0.000 description 1
238000002347 injection Methods 0.000 description 1
239000007924 injection Substances 0.000 description 1
231100000567 intoxicating Toxicity 0.000 description 1
230000002673 intoxicating effect Effects 0.000 description 1
235000020888 liquid diet Nutrition 0.000 description 1
238000012423 maintenance Methods 0.000 description 1
230000006996 mental state Effects 0.000 description 1
239000000203 mixture Substances 0.000 description 1
238000012986 modification Methods 0.000 description 1
230000004048 modification Effects 0.000 description 1
210000003205 muscle Anatomy 0.000 description 1
230000036640 muscle relaxation Effects 0.000 description 1
229960003086 naltrexone Drugs 0.000 description 1
DQCKKXVULJGBQN-XFWGSAIBSA-N naltrexone Chemical compound N1([C@@H]2CC3=CC=C(C=4O[C@@H]5[C@](C3=4)([C@]2(CCC5=O)O)CC1)O)CC1CC1 DQCKKXVULJGBQN-XFWGSAIBSA-N 0.000 description 1
239000002858 neurotransmitter agent Substances 0.000 description 1
230000007935 neutral effect Effects 0.000 description 1
231100000252 nontoxic Toxicity 0.000 description 1
230000003000 nontoxic effect Effects 0.000 description 1
238000001543 one-way ANOVA Methods 0.000 description 1
210000000056 organ Anatomy 0.000 description 1
230000000144 pharmacologic effect Effects 0.000 description 1
238000010149 post-hoc-test Methods 0.000 description 1
230000003389 potentiating effect Effects 0.000 description 1
239000000018 receptor agonist Substances 0.000 description 1
229940044601 receptor agonist Drugs 0.000 description 1
230000011514 reflex Effects 0.000 description 1
230000004044 response Effects 0.000 description 1
208000018198 spasticity Diseases 0.000 description 1
230000009154 spontaneous behavior Effects 0.000 description 1
230000002269 spontaneous effect Effects 0.000 description 1
238000007619 statistical method Methods 0.000 description 1
230000000707 stereoselective effect Effects 0.000 description 1
239000000126 substance Substances 0.000 description 1
239000000758 substrate Substances 0.000 description 1
230000009885 systemic effect Effects 0.000 description 1
230000001225 therapeutic effect Effects 0.000 description 1
230000003442 weekly effect Effects 0.000 description 1
238000005303 weighing Methods 0.000 description 1

Classifications

- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse

Landscapes

Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Addiction (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
Life Sciences & Earth Sciences (AREA)
Chemical & Material Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Neurology (AREA)
Psychiatry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Organic Chemistry (AREA)
Chemical Kinetics & Catalysis (AREA)
Neurosurgery (AREA)
Biomedical Technology (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
General Chemical & Material Sciences (AREA)
Epidemiology (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Preparation Of Compounds By Using Micro-Organisms (AREA)
Agricultural Chemicals And Associated Chemicals (AREA)

PL354083A 1999-10-08 2000-10-05 Zastosowanie baklofenu do wytwarzania leku PL200525B1 (pl)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
IT1999MI002107A IT1319275B1 (it)	1999-10-08	1999-10-08	Uso del baclofen nel trattamento dell'astinenza da etanolo.
PCT/EP2000/009750 WO2001026638A2 (en)	1999-10-08	2000-10-05	The use of baclofen in the treatment of alcoholism

Publications (2)

Publication Number	Publication Date
PL354083A1 PL354083A1 (en)	2003-12-29
PL200525B1 true PL200525B1 (pl)	2009-01-30

Family

ID=11383744

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
PL354083A PL200525B1 (pl)	1999-10-08	2000-10-05	Zastosowanie baklofenu do wytwarzania leku

Country Status (11)

Country	Link
EP (1)	EP1217999B1 (de)
AT (1)	ATE300295T1 (de)
AU (1)	AU7914600A (de)
CA (1)	CA2386817C (de)
DE (1)	DE60021590T2 (de)
DK (1)	DK1217999T3 (de)
ES (1)	ES2246900T3 (de)
HK (1)	HK1048062A1 (de)
IT (1)	IT1319275B1 (de)
PL (1)	PL200525B1 (de)
WO (1)	WO2001026638A2 (de)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US8048917B2 (en)	2005-04-06	2011-11-01	Xenoport, Inc.	Prodrugs of GABA analogs, compositions and uses thereof
KR20110097942A (ko)	2003-08-20	2011-08-31	제노포트 인코포레이티드	아실옥시알킬 카르바메이트 프로드러그, 합성 및 사용 방법
EP2354120A1 (de)	2003-08-20	2011-08-10	XenoPort, Inc.	Synthese von Acyloxyalkylcarbamat-Prodrugs und Zwischenprodukten davon
US7494985B2 (en)	2004-11-03	2009-02-24	Xenoport, Inc.	Acyloxyalkyl carbamate prodrugs, methods of synthesis, and use
US7566738B2 (en)	2004-11-03	2009-07-28	Xenoport, Inc.	Acyloxyalkyl carbamate prodrugs of sulfinic acids, methods of synthesis, and use
US7585996B2 (en)	2006-09-15	2009-09-08	Xenoport, Inc.	Acyloxyalkyl carbamate prodrugs, methods of synthesis and use
EP2250143B1 (de)	2008-01-25	2016-04-20	XenoPort, Inc.	Verfahren zur enzymatischen kinetischen racematspaltung von für die synthese von acyloxyalkylcarbamaten verwendeten acyloxyalkylthiocarbonaten
US7872046B2 (en)	2008-01-25	2011-01-18	Xenoport, Inc.	Crystalline form of a (3S)-aminomethyl-5-methyl-hexanoic acid prodrug and methods of use
WO2009094577A2 (en)	2008-01-25	2009-07-30	Xenoport, Inc.	Mesophasic forms of (3s)-aminomethyl-5-methyl-hexanoic acid prodrugs and methods of use
WO2010017498A1 (en)	2008-08-07	2010-02-11	Xenoport, Inc.	Methods of synthesizing n-hydroxysuccinimidyl carbonates
US8299291B2 (en)	2008-08-07	2012-10-30	Xenoport, Inc.	Methods of synthesizing 1-(acyloxy)-alkyl carbamate prodrugs
CA2753057C (en)	2009-03-03	2018-09-11	Xenoport, Inc.	Sustained release oral dosage forms of an r-baclofen prodrug
JP2012524065A (ja)	2009-04-17	2012-10-11	ゼノポート，インコーポレーテッド	ＧＡＢＡＢ受容体リガンドとしてのγ−アミノ酪酸誘導体
DE102010011069A1 (de)	2010-03-11	2011-09-15	Susanne Haamann	Verfahren zur gezielten pharmakologischen und co-psychotherapeutischen Behandlung der Alkoholabhängigkeit mit Baclofen und Nalmefen
WO2013023155A1 (en)	2011-08-11	2013-02-14	Xenoport, Inc.	Anhydrous and hemihydrate crystalline forms of an (r)-baclofen prodrug, methods of synthesis and methods of use
EP3244884A4 (de)	2015-01-15	2018-07-25	Allaysis, LLC	Intravenöse formulierungen von baclofen und behandlungsverfahren

1999
- 1999-10-08 IT IT1999MI002107A patent/IT1319275B1/it active
2000
- 2000-10-05 EP EP00969423A patent/EP1217999B1/de not_active Expired - Lifetime
- 2000-10-05 HK HK02109321.9A patent/HK1048062A1/zh unknown
- 2000-10-05 DK DK00969423T patent/DK1217999T3/da active
- 2000-10-05 PL PL354083A patent/PL200525B1/pl unknown
- 2000-10-05 CA CA002386817A patent/CA2386817C/en not_active Expired - Fee Related
- 2000-10-05 ES ES00969423T patent/ES2246900T3/es not_active Expired - Lifetime
- 2000-10-05 WO PCT/EP2000/009750 patent/WO2001026638A2/en not_active Ceased
- 2000-10-05 AT AT00969423T patent/ATE300295T1/de active
- 2000-10-05 DE DE60021590T patent/DE60021590T2/de not_active Expired - Lifetime
- 2000-10-05 AU AU79146/00A patent/AU7914600A/en not_active Abandoned

Also Published As

Publication number	Publication date
DK1217999T3 (da)	2005-11-28
WO2001026638A2 (en)	2001-04-19
DE60021590D1 (de)	2005-09-01
ITMI992107A1 (it)	2001-04-08
PL354083A1 (en)	2003-12-29
HK1048062A1 (zh)	2003-03-21
CA2386817C (en)	2009-05-12
AU7914600A (en)	2001-04-23
EP1217999B1 (de)	2005-07-27
ES2246900T3 (es)	2006-03-01
DE60021590T2 (de)	2006-05-24
WO2001026638A3 (en)	2002-02-28
ATE300295T1 (de)	2005-08-15
EP1217999A2 (de)	2002-07-03
CA2386817A1 (en)	2001-04-19
IT1319275B1 (it)	2003-09-26
ITMI992107A0 (it)	1999-10-08

Publication	Publication Date	Title
Ciccocioppo et al.	2002	Effect of selective blockade of μ1 or δ opioid receptors on reinstatement of alcohol-seeking behavior by drug-associated stimuli in rats
Mendelson et al.	1966	Serum cortisol levels in alcoholic and nonalcoholic subjects during experimentally induced ethanol intoxication
KR100533618B1 (ko)	2005-12-06	당뇨병 치료를 위한 방법 및 조성물
CA2386817C (en)	2009-05-12	The use of baclofen in the treatment of alcoholism
Rezvani et al.	1997	Attenuation of alcohol consumption by a novel nontoxic ibogaine analogue (18-methoxycoronaridine) in alcohol-preferring rats
JPH0432802B2 (de)	1992-06-01
Braun	1996	Buzz: the science and lore of alcohol and caffeine
Caputo et al.	2009	Incidence of craving for and abuse of gamma-hydroxybutyric acid (GHB) in different populations of treated alcoholics: an open comparative study
Riley et al.	2019	Schedule-induced polydipsia: is the rat a small furry human?(An analysis of an animal model of human alcoholism)
Bell et al.	1994	Ethanol reinforcement and its relationship to saccharin preference in Wistar rats
Zimmerberg et al.	1991	The effects of postnatal caffeine exposure on growth, activity and learning in rats
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Harris et al.	1978	Effects of d-amphetamine, monomethoxyamphetamines and hallucinogens on schedule-controlled behavior.
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JP2007195510A (ja)	2007-08-09	カロリー制限食品
Homewood et al.	1997	The effects of single and repeated episodes of thiamin deficiency on memory in alcohol-consuming rats
Xu et al.	2022	Peripheral and central pathophysiological changes in a new rat model of acid reflux combined with mental stress
Gentry et al.	1987	Why does a sucrose choice reduce the consumption of alcohol in C57BL/6J mice?
Pucilowski et al.	1994	Calcium channel inhibitors attenuate consumption of ethanol, sucrose and saccharin solutions in rats
Watson et al.	1987	Inhibited drinking and pica in rats following 2-deoxy-D-glucose
Gardell et al.	1998	Valproate reduces intake of alcoholic beverage among rats
Anylian, GH,* Dorn, J.* & Swerdlow	1978	The manifestations, aetiology and assessment of ethanol-induced hangover
RU2582966C2 (ru)	2016-04-27	Средство для снижения алкогольной мотивации при алкогольной зависимости
Hobson et al.	2018	Normal and abnormal intestinal absorption by humans
KR20090024215A (ko)	2009-03-06	인간의 성적 활동성을 향상시키기 위한 수단과 방법들